4.8 Article

Identification of Tumor Initiating Cells with a Small-Molecule Fluorescent Probe by Using Vimentin as a Biomarker

Journal

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 57, Issue 11, Pages 2851-2854

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201712920

Keywords

antitumor agents; biomarkers; cancer; fluorescent probes; high-throughput screening

Funding

  1. A*STAR (Agency for Science, Technology and Research, Singapore) Biomedical Research Council, Institute for Basic Science (IBS) [IBS-R007-A1]
  2. National Medical Research Council [NMRC/TCR/016-NNI/2016]

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Tumor initiating cells (TICs) have been implicated in clinical relapse and metastasis of a variety of epithelial cancers, including lung cancer. While efforts toward the development of specific probes for TIC detection and targeting are ongoing, a universal TIC probe has yet to be developed. We report the first TIC-specific fluorescent chemical probe, TiY, with identification of the molecular target as vimentin, a marker for epithelial-to-mesenchymal transition (EMT). TiY selectively stains TICs over differentiated tumor cells or normal cells, and facilitates the visualization and enrichment of functionally active TICs from patient tumors. At high concentration, TiY also shows anti-TIC activity with low toxicity to non-TICs. With the unexplored target vimentin, TiY shows potential as a first universal probe for TIC detection in different cancers.

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